Study on Biological Activity of Isoquinoline-Type Alkaloids

点击翻译按钮获取中文摘要

1. Biological Activity of Isoquinoline Alkaloids(1) Cytotoxicity of the Protoberberine-Type AlkaloidsCytotoxic activities of twenty four quaternary protoberberine alkaloids related to berberine have been evaluated using a human cancer cell line panel coupled with a drug sensitivity database. Extending the alkyl chain at position 8 or 13 strongly influenced the cytotoxic activity, that is, relative lipophilicity as well as the size of the substituent affects cytotoxicity. The highest level of activity was observed in 8- or 13-hexyl substituted derivatives of berberine.(2) Biological Activity of Simple Isoquinoline and Benzylisoquinoline AlkaloidsTwenty-six simple isoquinolines and 21 benzylisoquinolines were tested for antimicrobial, antimalarial, cytotoxic, and anti-HIV activities. Some simple isoquinoline alkaloids significantly active in each assay, and may be useful as lead compounds for developing potential chemotherapeutic agents. A quatemary nitrogen atom of isoquinolinium type m … More ay contribute to enhanced potency in the first three types activities. In contrast, anti-HIV activity was found with tetrahydroisoquinoline-type salts.(3) Fungicidal and Herbicidal Activities of Berberine Related AlkaloidsThe 23 quaternary and tertiary protoberberines related to berberine were tested for in vitro and/or in vivo fungicidal and herbicidal activities. Among the compounds tested, there was some activity observed with some of only the protoberberiniumsalts, but not sufficiently strong or broad spectrum for agrochemical utility. From the structure-activity point of view, some features can be pointed out.2. Structural Analysis of Alkaloid Metabolites in Cell Culture of Corydalis Species by LC/NMR and LC/MSThe biotransformations of 1-benzyltetrahydroisoquinolines in the cultured cells of Corydalis species were studied. Identification of metabolites was performed using LC/MS and LC/NMR techniques. These techniques enabled us to assign rapidly structures to these metabolites while avoiding the isolation of individual compounds. It was found that some metabolites were new 2, 3, 10, 11-oxygenated protoberberines. Less